Category: 25391-56-4

Foley, Daniel J. published the artcilePhenotyping Reveals Targets of a Pseudo-Natural-Product Autophagy Inhibitor, Formula: C5H4IN3O2, the main research area is indocinchona alkaloid synthesis palladium catalyzed annulation autophagy inhibitor; alkaloids; autophagy; chemical biology; inhibitors; natural products.

Pseudo-natural-product (NP) design combines natural product fragments to provide unprecedented NP-inspired compounds not accessible by biosynthesis, but endowed with biol. relevance. Since the bioactivity of pseudo-NPs may be unprecedented or unexpected, they are best evaluated in target agnostic cell-based assays monitoring entire cellular programs or complex phenotypes. Here, the Cinchona alkaloid scaffold was merged with the indole ring system to synthesize indocinchona alkaloids by Pd-catalyzed annulation. Exploration of indocinchona alkaloid bioactivities in phenotypic assays revealed a novel class of azaindole-containing autophagy inhibitors, the azaquindoles. Subsequent characterization of the most potent compound, azaquindole-1 (I), in the morphol. cell painting assay, guided target identification efforts. In contrast to the parent Cinchona alkaloids, azaquindoles selectively inhibit starvation- and rapamycin-induced autophagy by targeting the lipid kinase VPS34.

Angewandte Chemie, International Edition published new progress about Autophagy inhibitors. 25391-56-4 belongs to class iodides-buliding-blocks, name is 3-Iodo-5-nitropyridin-2-amine, and the molecular formula is C5H4IN3O2, Formula: C5H4IN3O2.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Bhat, Prasanna V. published the artcileEfficient and Scalable Process for Synthesis of 5-Nitro-7-azaindole, Computed Properties of 25391-56-4, the main research area is nitroazaindole preparation scalable process; nitrotrimethylsilanylethynylpyridinylamine preparation cycloisomerization; nitropyridinamine iodination Sonogashira reaction.

A simple and straightforward methodol. for the synthesis of 5-nitro-7-azaindole I has been developed using metal-free cycloisomerization of 5-nitro-3-trimethylsilanylethynyl-pyridin-2-ylamine. Large-scale applicability of this newly developed method was successfully demonstrated on multikilogram scale to obtain I in consistent yield and purity.

Organic Process Research & Development published new progress about Cycloisomerization. 25391-56-4 belongs to class iodides-buliding-blocks, name is 3-Iodo-5-nitropyridin-2-amine, and the molecular formula is C5H4IN3O2, Computed Properties of 25391-56-4.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Wang, Lei published the artcileModification of the aminopyridine unit of 2′-deoxyaminopyridinyl-pseudocytidine allowing triplex formation at CG interruptions in homopurine sequences, Quality Control of 25391-56-4, the main research area is aminopyridine derive sequence synthesis CG inversion site.

The antigene strategy based on site-specific recognition of duplex DNA by triplex DNA formation has been exploited in a wide range of biol. activities. However, specific triplex formation is mostly restricted to homo-purine strands within the target duplex DNA, due to the destabilizing effect of CG and TA inversion sites where there is an absence of natural nucleotides that can recognize the CG and TA base pairs. Hence, the design of artificial nucleosides, which can selectively recognize these inversion sites with high affinity, should be of great significance. Recently, we determined that 2-amino-3-methylpyridinyl pseudo-dC (3MeAP-VdC) possessed significant affinity and selectivity toward a CG inversion site and showed effective inhibition of gene expression. We now describe the design and synthesis of new modified aminopyridine derivatives by focusing on small chem. modification of the aminopyridine unit to tune and enhance the selectivity and affinity toward CG inversion sites. Remarkably, we have newly found that 2-amino-4-methoxypyridinyl pseudo-dC (4OMeAP-VdC) could selectively recognize the CG base pair in all four adjacent base pairs and form a stable triplex structure against the promoter sequence of the human gene including multiple CG inversion sites.

Nucleic Acids Research published new progress about Aminopyridines Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 25391-56-4 belongs to class iodides-buliding-blocks, name is 3-Iodo-5-nitropyridin-2-amine, and the molecular formula is C5H4IN3O2, Quality Control of 25391-56-4.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Seath, Ciaran P. published the artcileSynthesis of 2-BMIDA 6,5-bicyclic heterocycles by Cu(I)/Pd(0)/Cu(II) cascade catalysis of 2-iodoaniline/phenols, Recommanded Product: 3-Iodo-5-nitropyridin-2-amine, the main research area is BMIDA bicyclic heterocycle preparation; iodoaniline boronic acid MIDA ester heterocyclization copper palladium catalyst.

A one-pot cascade reaction for the synthesis of 2-BMIDA 6,5-bicyclic heterocycles has been developed using Cu(II)/Pd(0)/Cu(II) catalysis. 2-Iodoanilines and phenols undergo a Cu(I)/Pd(0)-catalyzed Sonogashira reaction with ethynyl BMIDA followed by in situ Cu(II)-catalyzed 5-endo-dig cyclization to generate heterocyclic scaffolds with a BMIDA functional group in the 2-position. The method provides efficient access to borylated indoles, benzofurans, and aza-derivatives, which can be difficult to access through alternative methods.

Chemical Communications (Cambridge, United Kingdom) published new progress about Heterocyclic compounds, nitrogen Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 25391-56-4 belongs to class iodides-buliding-blocks, name is 3-Iodo-5-nitropyridin-2-amine, and the molecular formula is C5H4IN3O2, Recommanded Product: 3-Iodo-5-nitropyridin-2-amine.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Wang, Lei published the artcileEffect of the 3-halo substitution of the 2′-deoxy aminopyridinyl-pseudocytidine derivatives on the selectivity and stability of antiparallel triplex DNA with a CG inversion site, SDS of cas: 25391-56-4, the main research area is deoxyaminopyridinyl pseudocytidine halo derivative antiparallel triplex DNA CG inversion; Antiparallel triplex DNA; Artificial nucleoside analogue; Inversion site; Non-natural type triplex DNA.

Triplex formation against a target duplex DNA has the potential to become a tool for genome research. However, there is an intrinsic restriction on duplex DNA sequences capable of forming the triplex DNA. Recently, we demonstrated the selective formation of the stable antiparallel triplexes containing CG inversion sites using a 2′-deoxy-1-methylpseudocytidine derivative (ΨdC), whose amino group was conjugated with the 2-aminopyridine at its 5-position as an addnl. H-bonding unit (AP-ΨdC). The 1-N position of 2-aminopyridine was supposed to be protonated to form the H-bond with the guanine of the CG inversion site. Here, to test the effect of the 3-substitution of the 2-aminopyridine unit of AP-ΨdC on triplex stability, we synthesized 3-halogenated 2-aminopyridine derivatives of AP-ΨdC. The pKa values of the 1-N position of the 2-aminopyridine unit of AP-ΨdC as the monomer nucleoside were determined to be 6.3 for 3-CH3 (MeAP-ΨdC), 6.1 for 3-H (AP-ΨdC), 4.3 for 3-Cl (ClAP-ΨdC), 4.4 for 3-Br (BrAP-ΨdC), and 4.7 for 3-I (IAP-ΨdC), suggesting that all of the halogenated AP-ΨdCs are not protonated under neutral conditions. Interestingly, although the recognition selectivity depends on the sequence context, the triplex-forming oligodeoxyribonucleotides (TFOs) having the sequence of the 3′-G-(IAP-ΨdC)-A-5′ context showed selective triplex formation with the CG inversion site. These results suggest that the protonation at the 1-N position plays an important role in the stable and selective triplex formation of AP-ΨdC derivatives in any sequences.

Bioorganic & Medicinal Chemistry published new progress about GC content. 25391-56-4 belongs to class iodides-buliding-blocks, name is 3-Iodo-5-nitropyridin-2-amine, and the molecular formula is C5H4IN3O2, SDS of cas: 25391-56-4.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com